Drugs

, Volume 46, Supplement 1, pp 129–133 | Cite as

Nimesulide in Dysmenorrhoea

  • M. Pulkkinen
Article

Summary

Nimesulide does not affect active intrauterine pressure, as measured using microsensors, or the direction and velocity of the propagation of uterine activity, but nevertheless alleviates pain significantly by 30 minutes after oral administration. In dysmenorrhoeic patients, resting pressure is high only in the fundus. Nimesulide reduces the pressure during the maximal but not during the submaximal pain period, with concomitant alleviation of pain. The drug changes the painful state of uterine contracture to painless cyclic contractions. With a single oral dose of 100mg, nimesulide is evenly distributed in female genital tissues (uterine fundus and cervix, oviduct and ovaries), reaching peak concentrations and peak plasma: tissue ratio (0.5) 3 hours after administration. Tissue concentrations range from 0.3 to 1.8.μg/g. Two 100mg oral doses of nimesulide administered to dysmenorrhoeic women in a double-blind placebo-controlled cross-over study reduced prostaglandin F levels in menstrual blood from 382 to 94 μg/L. Double-blind placebo-controlled studies also confirmed that nimesulide relieves pain in dysmenorrhoeic patients.

Keywords

Naproxen Nimesulide Mefenamic Acid Diflunisal Menstrual Blood 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Bevilacqua M, Magni E. Recent contributions to the knowledge of the mechanism of action of nimesulide. Drugs 46 (Suppl. 1): 40–47, 1993PubMedCrossRefGoogle Scholar
  2. Coren RL, Csapo AI. The intra-amniotic pressure. American Journal of Obstetrics and Gynecology 85: 470–483, 1963PubMedGoogle Scholar
  3. Csapo AI, Pulkkinen MO, Henzl M. The effect of naproxen-sodium on the intrauterine pressure and menstrual pain of dysmenorrheic patients. Prostaglandins 13: 193–199, 1977PubMedCrossRefGoogle Scholar
  4. Ekstrom P. Uterine activity and hyperactivity. Studies on the hormonal effects in the regulation of myometrial contractility and uterine blood flow of non-pregnant women with special regard to the mechanisms of dysmenorrhea. Acta Obstetricia et Gynecologica Scandinavica 71: 564–565, 1992CrossRefGoogle Scholar
  5. Maffei Facino R, Carini M, Aldini G. Antioxidant activity of nimesulide and its main metabolites. Drugs 46 (Suppl. 1): 15–21, 1993CrossRefGoogle Scholar
  6. Moggian G, Pellgri E, Tamburini E, Pini P, Tumidei U. A new treatment for primary dysmenorrhea. Clinica Therapeutica 117: 481–492, 1986Google Scholar
  7. Morrison JC, Nicolls ET. Epidemiological, social, and economical aspects of dysmenorrhea. In Dawood MY (Ed.) Dysmenorrhea, pp. 95–106, Williams & Wilkins, Baltimore, 1981Google Scholar
  8. Pelletier JP, Martel-Pelletier J. Effects of nimesulide and naproxen on the degradation and metalloprotease synthesis of human osteoarthritic cartilage. Drugs 46 (Suppl. 1): 34–39, 1993PubMedCrossRefGoogle Scholar
  9. Pulkkinen MO. Relief of menstrual discomfort and dysmenorrhea and simultaneous suppression of uterine activity by isoxepac. Acta Obstetricia et Gynecologica Scandinavica 59: 368–370, 1980CrossRefGoogle Scholar
  10. Pulkkinen MO. Diflunisal treatment before and during the dysmenorrheic period. In Diflunisal: profile of a modern analgesic, pp. 57–54, Waverly Press, Baltimore, 1982Google Scholar
  11. Pulkkinen MO. Alterations in intrauterine pressure, menstrual fluid prostaglandin F levels, and pain in dysmenorrheic women treated with nimesulide. Journal of Clinical Pharmacology 27: 65–69, 1987PubMedCrossRefGoogle Scholar
  12. Pulkkinen MO. Analysis of uterine contractility. In Garfield RE (Ed.) Uterine contractility, pp. 295–308, Serono Symposia, Norwell, 1990Google Scholar
  13. Pulkkinen MO, Csapo AI. Effect of ibuprofen on menstrual blood prostaglandin levels in dysmenhorrheic women. Prostaglandins 18: 137–142, 1979PubMedCrossRefGoogle Scholar
  14. Pulkkinen MO, Henzl M, Csapo AI. The effect of naproxen-sodium on the prostaglandin concentrations of the menstrual blood and ‘jet washings’ in dysmenorrheic women. Prostaglandins 15: 1055–1061, 1978PubMedCrossRefGoogle Scholar
  15. Pulkkinen M, Monti T, Macciocchi A. Analysis of uterine contractility after administration of the non-steroidal antiinflammatory drug nimesulide. Acta Obstetricia et Gynecologica Scandinavica 71: 181–185, 1992PubMedCrossRefGoogle Scholar
  16. Pulkkinen MO, Vuento M, Macciocchi A, Monti T. Distribution of oral nimesulide in female genital tissues. Biopharmaceutics and Drug Disposition 12: 113–117, 1991CrossRefGoogle Scholar
  17. Rondel RK, Eberhardt R, Koch J, Schuerman W. Treatment of primary essential dysmenorrhea with nimesulide in a double-blind cross-over study. Current Therapeutic Research 35: 123–129, 1984Google Scholar
  18. Ruponen S, Haataja M, Anttila M. Naproxen treatment in dysmenorrhea. Laakeuutiset 2: 43–45, 1978Google Scholar
  19. Verhoeven AJ, Tool ATJ, Kuijpers TW, Roos D. Nimesulide inhibits platelet-activating factor synthesis in activated human neutrophils. Drugs 46 (Suppl. 1): 52–58, 1993PubMedCrossRefGoogle Scholar

Copyright information

© ADIS International Limited 1993

Authors and Affiliations

  • M. Pulkkinen
    • 1
  1. 1.Department of Obstetrics and GynaecologyUniversity of TurkuTurkuFinland

Personalised recommendations